Structures of human SMG1-9 and SMG1-8-9 reveal how the SMG1 kinase active site is targeted by a specific inhibitor and provide insights into the regulation of the SMG1-8-9 kinase complex in nonsense-mediated mRNA decay.

Specific inhibition of cyclin-dependent kinase-like 5 (CDKL5), a kinase linked to a severe neurodevelopmental disorder, demonstrates an important role in the regulation of excitatory hippocampal synapses and synaptic plasticity that was not previously appreciated in rodent knock-out models.

A combination of NMR, fluorescence, and molecular dynamics simulations reveals the recognition mechanism for the intrinsically disordered regulator of protein kinase A, highlighting the enzyme's nuclear export process.

Slow conformational changes after drug binding rationalize selectivity, affinity and long on-target residence time for kinase inhibitors.

Combinations of inhibitors can more selectively inhibit individual or multiple protein kinases than single inhibitors.

The first-in-class kinase inhibitor, Ibrutinib, destabilizes its autoinhibited Bruton’s tyrosine kinase (BTK) target, and a remote resistance mutation causes global structural changes that activate BTK catalytic activity.

Orphan ATM kinase-domain missense mutations are unexpectedly common and form a potent oncogenic event and a biomarker for Topo-isomerase I inhibitor based therapy.

An FDA-approved, rho-associated kinase inhibitor reverses fibrosis in the conventional outflow pathway of a mouse model of glaucoma and reverses ocular hypertension in patients with steroid glaucoma.

Rescue of DUX4-induced muscle pathology by the RET inhibitor Sunitinib reveals the therapeutic potential for treatment of Facioscapulohumeral muscular dystrophy using tyrosine kinase inhibitors.